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1. 发明授权

US5505784A Polycondensates which contain tartaric acid derivatives, processes for their preparation and use thereof 失效
标题翻译：含有酒石酸衍生物的缩聚物，其制备方法和用途
公开(公告)号：US5505784A
公开(公告)日：1996-04-09
申请号：US370885
申请日：1995-01-10
申请人： Volker Krone , Michael Magerstadt , Axel Walch , Gunter Ditzinger , Norbert Lill
发明人： Volker Krone , Michael Magerstadt , Axel Walch , Gunter Ditzinger , Norbert Lill
IPC分类号： A61K31/765 , A61K9/16 , A61K9/20 , A61K9/22 , A61K31/785 , A61K31/795 , A61K49/22 , C08G63/16 , C08G63/60 , C08G63/66 , C08G63/68 , C08G69/26 , C08G75/00 , C08G75/26 , A61B8/14
CPC分类号： C08G63/66 , A61K49/225 , A61K9/1641 , A61K9/1647 , A61K9/204 , A61K9/2045 , C08G63/16 , C08G63/60 , C08G63/68 , C08G69/26
摘要： The invention relates to polycondensates which consist of at least 95 mol % of recurring structural units of the formula I ##STR1## where R.sup.1 is a 2,3-O-alkylidenetartaric acid derivative (II) or furo[2,5] (V), alkyl, alkenyl, cycloalkyl, cycloalkenyl, aryl or a heterocycle, X is --O--, --NH-- or --S-- and R.sup.2 is 2,3-O-alkylidene-L-threitol (III) or a compound of the formula VI, alkyl, alkenyl, cycloalkyl, cycloalkenyl, aryl or a heterocycle, with the proviso that more than 5 mol % of the radicals R.sup.1 and/or R.sup.2 are present in the polycondensate of the formula I, where R.sup.1 is compound of the formula II or R.sup.2 is a compound of the formula III or R.sup.1 is a compound of the formula II and R.sup.2 is a compound of the formula III, or in which more than 5 mol % of the radicals R.sup.1 and R.sup.2 are present in the polycondensate of the formula I, wherea) R.sup.1 is a compound of the formula V and R.sup.2 is a compound of the formula VI, orb) R.sup.1 is phenyl[1,2], phenyl[1,3] or phenyl[1,4] and R.sup.2 is a compound of the formula VI,to a process for the preparation of these polycondensates, and to their use for the production of depot preparations with controlled release of active substance or for the production of ultrasonic contrast agents.
摘要翻译：本发明涉及由至少95摩尔％的式I（I）的重复结构单元组成的缩聚物，其中R 1是2,3-O-亚烷基二十二烷酸衍生物（II）或呋喃并[2,5] （V），烷基，烯基，环烷基，环烯基，芳基或杂环，X是-O-，-NH-或-S-，R2是2,3-O-亚烷基-L-苏糖醇（III）式VI的烷基，烯基，环烷基，环烯基，芳基或杂环，条件是在式I的缩聚物中存在大于5摩尔％的基团R 1和/或R 2，其中R 1是式II或R2是式III化合物或R1是式II化合物，R2是式III化合物，或其中基团R1和R2多于5mol％存在于缩聚物中其中a）R 1是式V的化合物，R 2是式VI的化合物，或b）R 1是苯基[1,2]，苯基[1,3]或苯基[1,4 并且R 2是式V的化合物本发明涉及一种制备这些缩聚物的方法，以及它们用于生产具有活性物质的控制释放或用于生产超声造影剂的贮库制剂的用途。

2. 发明授权

US5700459A Pharmacological composition containing polyelectrolyte complexes in microparticulate form and at least one active agent 失效
标题翻译：含有微粒形式的聚电解质复合物和至少一种活性剂的药理组合物
公开(公告)号：US5700459A
公开(公告)日：1997-12-23
申请号：US341164
申请日：1994-11-16
申请人： Volker Krone , Michael Magerstadt , Axel Walch , Albrecht Groner , Dieter Hoffmann
发明人： Volker Krone , Michael Magerstadt , Axel Walch , Albrecht Groner , Dieter Hoffmann
IPC分类号： A61K9/107 , A61K9/14 , A61K9/16 , A61K9/50 , A61K38/00 , A61K39/00 , A61K45/00 , A61K47/36 , A61K47/42 , A61K49/00 , A61K49/08 , A61K49/22 , A61P35/00 , A61P43/00 , G09B23/28
CPC分类号： G09B23/286 , A61K49/223 , A61K9/1641 , A61K9/1652 , Y10S514/951
摘要： The invention relates to a pharmacological composition comprising a polyelectrolyte complex, in particular a polyacid with an average particle size of less than 15 .mu.m and an active agent, among which are active peptides, proteins, enzymes, enzyme inhibitors, antigens, cytostatics, antiinflamatory agents, antibiotics and vaccines. The said composition ensures that the active agent is converted in a non-deleterious manner into a form which can be administered. In addition, the biodistribution, bioavailability and absorption of the pharmaceutical are beneficially affected.
摘要翻译：本发明涉及包含聚电解质复合物，特别是平均粒度小于15μm的多酸和活性剂的药物组合物，其中有活性肽，蛋白质，酶，酶抑制剂，抗原，细胞抑制剂，抗炎药药剂，抗生素和疫苗。所述组合物确保活性剂以非有害的方式转化成可以施用的形式。此外，药物的生物分布，生物利用度和吸收受到有益的影响。

3. 发明授权

US5219555A Method for labeling proteins with technetium or rhenium 失效
标题翻译：用技术或铑标记蛋白质的方法
公开(公告)号：US5219555A
公开(公告)日：1993-06-15
申请号：US236401
申请日：1988-08-25
申请人： Karl-Heinz Bremer , Ludwig Kuhlmann , Michael Magerstadt , Alexander Schwarz , Axel Steinstrasser
发明人： Karl-Heinz Bremer , Ludwig Kuhlmann , Michael Magerstadt , Alexander Schwarz , Axel Steinstrasser
IPC分类号： A61K51/00 , A61K51/04 , C07B31/00 , C07B59/00 , C07C67/00 , C07D257/02 , C07F13/00
CPC分类号： C07F13/005 , A61K51/0482 , A61K51/0497 , C07D257/02 , A61K2121/00 , A61K2123/00
摘要： The invention relates to a method for labeling substances with--in particular radioactive--technetium or rhenium isotopes with the aid of N-substituted or C-substituted macrocyclic amine derivatives of the formula I and/or II ##STR1## in which R.sup.1 -R.sup.7, Y, m, n, o, p, f, g, h, i and j have the stated meanings, and to the use of these labeled substances, especially in medical diagnosis.
摘要翻译：本发明涉及一种借助于式I和/或II的N-取代或C取代的大环胺衍生物，特别是放射性锝或铼同位素来标记物质的方法。哪些R1-R7，Y，m，n，o，p，f，g，h，i和j具有所述的含义，以及这些标记物质的使用，特别是在医学诊断中。

4. 发明授权

US5190982A Ultrasonic contrast agents, processes for their preparation and the use thereof as diagnostic and therapeutic agents 失效
公开(公告)号：US5190982A
公开(公告)日：1993-03-02
申请号：US859257
申请日：1992-05-26
申请人： Raimund Erbel , Rainer Zotz , Volker Krone , Michael Magerstadt , Axel Walch
发明人： Raimund Erbel , Rainer Zotz , Volker Krone , Michael Magerstadt , Axel Walch
IPC分类号： G09F13/04 , H02B15/00
CPC分类号： H02B15/00 , G09F2013/0427
摘要： The invention relates to ultrasonic contrast agents composed of microparticles which contain a gas and polyamino-dicarboxylic acid-co-imide derivatives, to processes for their preparation and to their use as diagnostic and therapeutic agents.

5. 发明授权

US5205287A Ultrasonic contrast agents, processes for their preparation and the use thereof as diagnostic and therapeutic agents 失效
标题翻译：超声造影剂，其制备方法及其用作诊断和治疗剂
公开(公告)号：US5205287A
公开(公告)日：1993-04-27
申请号：US955146
申请日：1992-10-01
申请人： Raimund Erbel , Rainer Zotz , Volker Krone , Michael Magerstadt , Axel Walch
发明人： Raimund Erbel , Rainer Zotz , Volker Krone , Michael Magerstadt , Axel Walch
IPC分类号： A61K49/22
CPC分类号： A61K49/223
摘要： The invention relates to ultrasonic contrast agents composed of microparticles which contain a gas and polyamino-dicarboxylic acid-co-imide derivatives, to processes for their preparation and to their use as diagnostic and therapeutic agents.
摘要翻译：本发明涉及由含有气体和聚氨基二羧酸 - 共 - 酰亚胺衍生物的微粒组成的超声造影剂，其制备方法及其作为诊断和治疗剂的用途。

6. 发明授权

US5137928A Ultrasonic contrast agents, processes for their preparation and the use thereof as diagnostic and therapeutic agents 失效
标题翻译：超声对比剂，其制备方法及其作为诊断和治疗剂的用途
公开(公告)号：US5137928A
公开(公告)日：1992-08-11
申请号：US690761
申请日：1991-04-24
申请人： Raimund Erbel , Rainer Zotz , Volker Krone , Michael Magerstadt , Axel Walch
发明人： Raimund Erbel , Rainer Zotz , Volker Krone , Michael Magerstadt , Axel Walch
IPC分类号： A61K31/785 , A61K49/00 , A61K49/22 , A61P43/00 , C08G69/10
CPC分类号： A61K49/223
摘要： The invention relates to ultrasonic contrast agents composed of microparticles which contain a gas and polyamino-dicarboxylic acid-co-imide derivatives, to processes for their preparation and to their use as diagnostic and therapeutic agents.
摘要翻译：本发明涉及由含有气体和聚氨基 - 二羧酸 - 共 - 酰亚胺衍生物的微粒组成的超声造影剂，其制备方法及其作为诊断和治疗剂的用途。

7. 发明授权

US5106740A Immobilization of an isethiacyanate of a cofactor on a polymer 失效
标题翻译：聚合物上的凝血酶的异柠檬酸的固定化
公开(公告)号：US5106740A
公开(公告)日：1992-04-21
申请号：US622115
申请日：1990-12-06
申请人： Hubert Bader , Hans-Ullrich Hoppe , Michael Magerstadt , Merten Schlingmann , Dieter Ulschneider , Axel Walch
发明人： Hubert Bader , Hans-Ullrich Hoppe , Michael Magerstadt , Merten Schlingmann , Dieter Ulschneider , Axel Walch
IPC分类号： C07H19/207 , C12M1/40 , C12N11/04 , C12N11/08
CPC分类号： C12M21/18 , C07H19/207 , C12M25/02 , C12N11/04 , C12N11/08
摘要： A cofactor having an aromatic or benzylic amino group is converted into an isothiocyanate by reaction with a compound such as thiophosgene and the isothiocyanate of the cofactor is attached to a polymer which is preferably water-soluble. When the polymer has amino groups, a thiourea bridge is formed between the polymer and cofactor and a polymer having hydroxyl groups results in a thiocarbamate bridge. The polymer may be a copolymer of vinylamine or vinylmethylamine and vinylmethylacetamide, partially alkylamine-substituted .alpha., .beta.-poly-(2-hydroxyethyl)-D,L-aspartamide, polyethyleneimine or carbohydrate. The cofactor bound to a polymer and an enzyme are contained in microcapsules or in a membrane to form an enzyme reactor.
摘要翻译：具有芳族或苄基氨基的辅因子通过与化合物例如硫代光气反应而转化成异硫氰酸酯，辅因子的异硫氰酸酯连接到优选水溶性的聚合物上。当聚合物具有氨基时，在聚合物和辅因子之间形成硫脲桥，并且具有羟基的聚合物导致硫代氨基甲酸酯桥。聚合物可以是乙烯胺或乙烯基甲胺和乙烯基甲基乙酰胺，部分烷基胺取代的+60，β-聚 - （2-羟乙基）-D，L-天冬酰胺，聚乙烯亚胺或碳水化合物的共聚物。与聚合物和酶结合的辅因子包含在微胶囊或膜中以形成酶反应器。

8. 发明授权

US5391696A Polycondensates which contain tartaric acid derivatives, processes for their preparation and use thereof 失效
标题翻译：含有酒石酸衍生物的缩聚物，其制备方法和用途
公开(公告)号：US5391696A
公开(公告)日：1995-02-21
申请号：US886197
申请日：1992-05-21
申请人： Volker Krone , Michael Magerstadt , Axel Walch , Gunter Ditzinger , Norbert Lill
发明人： Volker Krone , Michael Magerstadt , Axel Walch , Gunter Ditzinger , Norbert Lill
IPC分类号： A61K31/765 , A61K9/16 , A61K9/20 , A61K9/22 , A61K31/785 , A61K31/795 , A61K49/22 , C08G63/16 , C08G63/60 , C08G63/66 , C08G63/68 , C08G69/26 , C08G75/00 , C08G75/26 , C08G69/44
CPC分类号： C08G63/66 , A61K49/225 , A61K9/1641 , A61K9/1647 , A61K9/204 , A61K9/2045 , C08G63/16 , C08G63/60 , C08G63/68 , C08G69/26
摘要： Polycondensates which contain tartaric acid derivatives, processes for their preparation and use thereof.The invention relates to polycondensates which consist of at least 95 mol % of recurring structural units of the formula I ##STR1## where R.sup.1 is a 2,3-O-alkylidenetartaric acid derivative (II) or furo[2,5] (V), alkyl, alkenyl, cycloalkyl, cycloalkenyl, aryl or a heterocycle, X is --O--, --NH-- or --S-- and R.sup.2 is 2,3-O-alkylidene-L-threitol (III) or a compound of the formula VI, alkyl, alkenyl, cycloalkyl, cycloalkenyl, aryl or a heterocycle, with the proviso that more than 5 mol % of the radicals R.sup.1 and/or R.sup.2 are present in the polycondensate of the formula I, where R.sup.1 is compound of the formula II or R.sup.2 is a compound of the formula III or R.sup.1 is a compound of the formula II and R.sup.2 is a compound of the formula III, or in which more than 5 mol % of the radicals R.sup.1 and R.sup.2 are present in the polycondensate of the formula I, wherea) R.sup.1 is a compound of the formula V and R.sup.2 is a compound of the formula VI, orb) R.sup.1 is phenyl[1,2], phenyl[1,3] or phenyl[1,4] and R.sup.2 is a compound of the formula VI,to a process for the preparation of these polycondensates, and to their use for the production of depot preparations with controlled release of active substance or for the production of ultrasonic contrast agents.
摘要翻译：含有酒石酸衍生物的缩聚物，其制备方法和用途。本发明涉及由至少95摩尔％的式I（I）的重复结构单元组成的缩聚物，其中R 1是2,3-O-亚烷基二苯甲酸衍生物（II）或呋喃并[2,5] （V），烷基，烯基，环烷基，环烯基，芳基或杂环，X是-O-，-NH-或-S-，R2是2,3-O-亚烷基-L-苏糖醇（III）式VI的烷基，烯基，环烷基，环烯基，芳基或杂环，条件是在式I的缩聚物中存在大于5摩尔％的基团R 1和/或R 2，其中R 1是式II或R2是式III化合物或R1是式II化合物，R2是式III化合物，或其中基团R1和R2多于5mol％存在于缩聚物中其中a）R 1是式V的化合物，R 2是式VI的化合物，或b）R 1是苯基[1,2]，苯基[1,3]或苯基[1,4 并且R 2是式V的化合物本发明涉及一种制备这些缩聚物的方法，以及它们用于生产具有活性物质的控制释放或用于生产超声造影剂的贮库制剂的用途。

9. 发明授权

US4835248A Biologically degradable polyamide for depot preparations having controlled release of the active compound 失效
标题翻译：用于具有活性化合物的控制释放的贮库制剂的生物可降解聚酰胺
公开(公告)号：US4835248A
公开(公告)日：1989-05-30
申请号：US49164
申请日：1987-05-13
申请人： Hubert Bader , Diether Ruppel , Axel Walch , Michael Magerstadt
发明人： Hubert Bader , Diether Ruppel , Axel Walch , Michael Magerstadt
IPC分类号： A61K9/00 , A61K9/16 , A61K9/20 , A61K9/22 , A61K47/00 , A61K47/34 , C08G69/02 , C08G69/10 , C08G69/44
CPC分类号： C08G69/44 , A61K9/1641 , A61K9/2045 , C08G69/02 , C08G69/10
摘要： Polyamides in which amino acids are incorporated in the polymer backbone via two amino or carboxyl groups and which carry in the .alpha.-position to the amide structure a functional group which is responsible for degradation and active compound release are highly suitable for the preparation of biologically degradable active compound depot preparations having controlled release of the active compound.
摘要翻译：通过两个氨基或羧基将氨基酸并入聚合物主链中并且其与酰胺结构的α位相结合的聚酰胺是负责降解和活性化合物释放的官能团，非常适用于生物可降解的活性化合物贮库制剂具有控释活性化合物。

10. 发明授权

US5613494A Polycondensates which contain tartaric acid derivatives, processes for their preparation and use thereof 失效
标题翻译：含有酒石酸衍生物的缩聚物，其制备方法和用途
公开(公告)号：US5613494A
公开(公告)日：1997-03-25
申请号：US435115
申请日：1995-05-04
申请人： Volker Krone , Michael Magerstadt , Axel Walch , Gunter Ditzinger , Norbert Lill
发明人： Volker Krone , Michael Magerstadt , Axel Walch , Gunter Ditzinger , Norbert Lill
IPC分类号： A61K31/765 , A61K9/16 , A61K9/20 , A61K9/22 , A61K31/785 , A61K31/795 , A61K49/22 , C08G63/16 , C08G63/60 , C08G63/66 , C08G63/68 , C08G69/26 , C08G75/00 , C08G75/26 , A61B8/14
CPC分类号： C08G63/66 , A61K49/225 , A61K9/1641 , A61K9/1647 , A61K9/204 , A61K9/2045 , C08G63/16 , C08G63/60 , C08G63/68 , C08G69/26
摘要： Polycondensates which contain tartaric acid derivatives, processes for their preparation and use thereof.The invention relates to polycondensates which consist of at least 95 mol % of recurring structural units of the formula I ##STR1## where R.sup.1 is a 2,3-O-alkylidenetartaric acid derivative (II) or furo[2,5] (V), alkyl, alkenyl, cycloalkyl, cycloalkenyl, aryl or a heterocycle, X is --O-- --NH-- or --S-- and R.sup.2 is 2,3-O-alkylidene-L-threitol (III) or a compound of the formula VI, alkyl, alkenyl, cycloalkyl, cycloalkenyl, aryl or a heterocycle, with the proviso that more than 5 mol % of the radicals R.sup.1 and/or R.sup.2 are present in the polycondensate of the formula I, where R.sup.1 is compound of the formula II or R.sup.2 is a compound of the formula III or R.sup.1 is a compound of the formula II and R.sup.2 is a compound of the formula III, or in which more than 5 mol % of the radicals R.sup.1 and R.sup.2 are present in the polycondensate of the formula I, wherea) R.sup.1 is a compound of the formula V and R.sup.2 is a compound pound of the formula VI, orb) R.sup.1 is phenyl[1,2], phenyl[1,3]or phenyl[1,4]and R.sup.2 is a compound of the formula VI,to a process for the preparation of these polycondensates, and to their use for the production of depot preparations with controlled release of active substance or for the production Of ultrasonic contrast agents.
摘要翻译：含有酒石酸衍生物的缩聚物，其制备方法和用途。本发明涉及由至少95摩尔％的式I（I）的重复结构单元组成的缩聚物，其中R 1是2,3-O-亚烷基二苯甲酸衍生物（II）或呋喃并[2,5] （V），烷基，链烯基，环烷基，环烯基，芳基或杂环，X是-O-NH-或-S-，R 2是2,3-O-亚烷基-L-苏糖醇（III）式VI，烷基，烯基，环烷基，环烯基，芳基或杂环，条件是在式I的缩聚物中存在大于5mol％的基团R 1和/或R 2，其中R 1是式II或R2是式III的化合物或R 1是式II的化合物，R 2是式III的化合物，或其中大于5mol％的基团R 1和R 2存在于缩合物的缩聚物中式I，其中a）R 1是式V的化合物，R 2是式VI的化合物，或b）R 1是苯基[1,2]，苯基[1,3]或苯基[1,4 并且R 2是下式的化合物 VI，用于制备这些缩聚物的方法，以及它们用于生产具有活性物质的控制释放或用于生产超声造影剂的贮库制剂的用途。

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